Potential of Polygonum cuspidatum Root as an Antidiabetic Food: Dual High-Resolution α-Glucosidase and PTP1B Inhibition Profiling Combined with HPLC-HRMS and NMR for Identification of Antidiabetic Constituents

• DOI: 10.1021/acs.jafc.7b01353
• Publication Date: 2017-05-12T15:33:17Z
• Authors: Yong Zhao; Martin Xiaoyong Chen; Kenneth Thermann ...; Anna Katharina Jäger; Dan Staerk
• Keywords: Polygonum

The worldwide increasing incidence of type 2 diabetes has fueled an intensified search for food and herbal remedies with preventive and/or therapeutic properties. Polygonum cuspidatum Siebold & Zucc. (Polygonaceae) is used as a functional in Japan South Korea, it also well-known traditional antidiabetic herb China. In this study, dual high-resolution α-glucosidase protein-tyrosine phosphatase 1B (PTP1B) inhibition profiling was the identification individual constituents directly from crude ethyl acetate extract fractions P. cuspidatum. Subsequent preparative-scale HPLC to isolate series inhibitors, which after HPLC-HRMS NMR analysis were identified procyanidin B2 3,3″-O-digallate (3) (-)-epicatechin gallate (5) IC50 values 0.42 ± 0.02 0.48 0.0004 μM, respectively, well stilbene analogues value range 6.05 0.05 116.10 2.04 μM. addition, (trans)-emodin-physcion bianthrone (15b) (cis)-emodin-physcion (15c) potent PTP1B inhibitors 2.77 1.23 7.29 2.32 respectively. These findings show that potential management diabetes.